Study of the anticancer potential of Yemeni plants used in folk medicine

The present work evaluated the anticancer activity of methanol extracts from 24 plants used in Yemeni traditional medicine. To evaluate the in vitro cytotoxic potency of the investigated extracts, an established microtiter plate assay based on cellular staining with crystal violet was used with 5 human cancer cell lines: two lung cancer (A-427 and LCLC-103H), two urinary bladder carcinoma (5637 and RT-112) and one breast cancer (MCF-7) line. The methanolic extracts of Dendrosicyos socotrana, Withanina aduensis, Withania riebeckii, Dracena cinnabari and Buxus hildebrandtii exhibited the highest toxicity on all tumor cell lines with IC50 values ranging between 0.29 and 5.54 microg/ml. The extracts of Jatropha unicostata and Punica protopunica showed a moderate potency on the most tumor cell lines.     

Evaluation and Comparison of the In Vitro Cytotoxic Activity of Withania somnifera Methanolic and Ethanolic Extracts against MDA-MB-231 and Vero Cell Lines

Withania somnifera Dunal (WS), commonly known as Ashwagandha in India, belongs to the family Solanaceae. It is extensively used in most of the Indian herbal pharmaceuticals and nutraceuticals. In the current study, the in vitro cytotoxic activity of methanolic, ethanolic, and aqueous extracts of WS stems was evaluated using cytometry and the MTT assay against the MDA-MB-231 human breast cancer cell line. Methanolic and ethanolic extracts of WS showed potent anticancer activity on the MDA-MB-231 human breast cancer cell line, whereas the aqueous extract did not exhibit any significant activity at 100 µg/ml. The percentage viability of the cell lines was determined by using the Trypan blue dye exclusion method. Cell viability was reduced to 21% and 0% at 50 and 100 µg/ml of the methanolic extract, respectively, as compared to 19% and 0% at 50 and 100 µg/ml for the ethanolic extract and 37% at 100 µg/ml in sterile Milli-Q water after 48 hours of treatment. Methanolic and ethanolic extracts of WS were shown to possess IC₅₀ values of 30 and 37 µg/ml, respectively, by the MTT assay and cytometer-based analysis, with the methanolic extract being more active than the other two. On the other hand, methanolic and ethanolic extracts of WS did not exhibit any significant in vitro activity against the normal epithelial cell line Vero at 50 µg/ml. HPLC was carried out for the analysis of its phytochemical profile and demonstrated the presence of the active component Withaferin A in both extracts. The methanolic and ethanolic extracts of Withania should be studied further for the isolation and characterization of the active components to lead optimization studies.     

Antiproliferative activity of plant extracts used against cancer in traditional medicine

Forty four extracts from sixteen plants used traditionally as anticancer agents were evaluated in vitro for their antiproliferative activity against Hep-2, MCF-7, and Vero cell lines. Plants were fractionated using ethanol, methanol, chloroform, n-hexane, distilled water, and butanol. The antiproliferative activity was measured by MTT assay. TLC was used to identify active fractions. The apoptotic activity of active fractions was determined using TUNEL colorimetric assay. 20 of these extracts demonstrated significant antiproliferative activity against one or more of the cell lines. These extracts were prepared from Ononis hirta, Inula viscosa, Salvia pinardi, Verbascum sinaiticum and Ononis sicula. Methanol fractions of Ononis hirta (aerial parts) and Inula viscosa (flowers) were the most active fractions against MCF-7 cells with IC₅₀ of 27.96 and 15.78 μg/ml respectively and they were less toxic against other cell lines. Other extracts showed lower activity against cancer cell lines. TLC analysis showed the presence of flavonoids and terpenoids in active plants while alkaloids were detected in Ononis hirta (aerial parts) extracts. Ononis hirta (aerial parts) and Inula viscosa (flowers) extracts exerted their antiproliferative activity by inducing apoptosis in cancer cell lines. Further studies are necessary for detailed chemical characterization and more extensive biological evaluation of the most active ingredients.     

Separation and Quantification of Tiliroside from Plant Extracts by SPE/RP-HPLC

Kaempferol-3-O-β-D-(6″-E-p-coumaroyl)-glucopyranoside (tiliroside) has been isolated from many natural plants sources. This compound showed very interesting pharmacological activities, e.g., cytotoxic for human leukaemic cell lines and anti-complement activity. However, there is a lack of data concerning the presence of this compound in medical plants. In this work, a reproducible and quick method was elaborated for the separation and determination of tiliroside in methanolic extracts of the plants. Solid-phase extraction was applied as sample preparation technique for the purification of crude extracts from various species as well as for the isolation of tiliroside for further reversed-phase high performance liquid chromatography analysis. The content of tiliroside for various plant materials was compared.     

Evaluation of native and exotic Brazilian plants for anticancer activity

Native and exotic Brazilian plants collected in the State of Minas Gerais were evaluated for their anticancer potential. Methanol extracts from leaves of 51 plant species were tested for cytotoxicity against four tumor cell lines: B16 (murine skin), HL-60 (human leukemia), MCF-7 (human breast), and HCT-8 (human colon). Plant extracts that exhibited IC₅₀ values less than 30 μg/ml against any tumor cell line were tested on sea urchin egg development and mouse erythrocytes. In addition, all extracts were evaluated for their general toxicity using the brine shrimp lethality assay. The most active extracts against the tumor cells were those obtained from Lantana fucata, Copaifera langsdorffii, and Momordica charantia. These three extracts inhibited sea urchin development from the first cleavage, but those from C. langsdorffii and M. charantia were very active against mouse erythrocytes. Only the L. fucata extract presented no hemolytic activity. Consequently, although the extracts of L. fucata, M. charantia, and C. langsdorffii could be useful in the development of new anticancer products, the first of these extracts is the most promising since it did not present unspecific toxicity, as suggested by negative results obtained with brine shrimp lethality and mouse erythrocytes assays.     

Antiplasmodial and antitrypanosomal activity of plants from the Kingdom of Saudi Arabia

The antiplasmodial and antitrypanosomal activity of the methanol extracts of 42 plants collected from the Kingdom of Saudi Arabia and some fractions obtained thereof were evaluated. The antiplasmodial activity was tested in vitro against chloroquine-resistant strain (K1) and sensitive strain (FCR3), and the antitrypanosomal activity was tested in vitro against Trypanosoma brucei brucei GUTat 3.1 strain. For host cells, the cytotoxicity of the active extracts was also evaluated against the MRC5 human cell line. Only extracts of three samples demonstrated good antiplasmodial activity (IC₅₀ < 12.5 and > 1.56 μg/ml, score 2), the methanol extracts of Lycium shawii, Heliotropium zeylanicum and the petroleum ether-soluble fraction of the methanol extract of Caralluma tuberculata, while extracts of the remaining 42 plants were inactive (IC₅₀ > 12.5 μg/ml, score 1). As for the antitrypanosomal activity, the methanol extract of Solanum schimperianum demonstrated the highest activity (IC₅₀ 0.061 μg/ml), followed by the petroleum ether-soluble fraction of the methanol extract of C. tuberculata (IC₅₀ 0.5 μg/ml). The chloroform-soluble fraction of the methanol extract of C. tuberculata was moderately active (IC₅₀ 3.5 μg/ml), with low cytotoxicity (IC₅₀ 62.6 μg/ml) and moderate selectivity index (SI 17.9). The methanolic extracts of 34 plants showed good activity with score 2 (IC₅₀ < 12.5 and > 1.56 μg/ml), while the extracts of seven plants were inactive (IC₅₀ > 12.5 μg/ml, score 1).     

Anti-tumour activity of Digitalis purpurea L. subsp. heywoodii

Recent research has shown the anticancer effects of digitalis compounds suggesting their possible use in medical oncology. Four extracts obtained from the leaves of Digitalis purpurea subsp. heywoodii have been assessed for cytotoxic activity against three human cancer cell lines, using the SRB assay. All of them showed high cytotoxicity, producing IC50 values in the 0.78 - 15 microg/mL range with the methanolic extract being the most active, in non toxic concentrations. Steroid glycosides (gitoxigenin derivatives) were detected in this methanolic extract. Gitoxigenin and gitoxin were evaluated in the SRB assay using the three human cancer cell lines, showing IC50 values in the 0.13 - 2.8 microM range, with the renal adenocarcinoma cancer cell line (TK-10) being the most sensitive one. Morphological apoptosis evaluation of the methanolic extract and both compounds on the TK-10 cell line showed that their cytotoxicity was mediated by an apoptotic effect. Finally, possible mechanisms involved in apoptosis induction by digitalis compounds are discussed.     

Assessment of selected Yemeni medicinal plants for their in vitro antimicrobial,anticancer, and antioxidant activities

Context: The role of natural products as a source for remedies has been recognized since the beginning of mankind. Nevertheless, a minority of folkloricly used medicinal plants have been evaluated for their pharmacological activities.

Objectives: The purpose of this study is to evaluate 33 selected Yemeni plants for their in vitro anticancer, antimicrobial, and antioxidant activities.

Materials and methods: The plants were extracted with methanol and hot water. The obtained 66 extracts were tested for their in vitro cytotoxic activity using the neutral red uptake assay against two cancer cell lines (5637 and MCF-7). The antimicrobial activity was determined using the agar diffusion method and MIC-determination. The DPPH radical method was used for the determination of antioxidant activity.

Results: Interesting cytotoxic activity was observed for Hypoestes forskalei (Vahl) R. Br. (Acanthaceae), Lycium shawii Roem. & Schult. (Solanaceae), Pergularia tomentosa L. (Asclepiadaceae), Psiadia punctulata (DC.) Vatke (Compositae), Pulicaria petiolaris Jaub. & Spach (Compositae) and Rosmarinus officinalis L. (Labiatae) (IC₅₀ values < 50 μg/mL). Antimicrobial activity with MIC values ≤ 125 μg/mL was exhibited against Gram-positive bacteria by Chrozophora oblongifolia (Del.) A.Juss. ex Spreng. (Euphorbiaceae), Myrtus communis L. (Myrtaceae), Phragmanthera regularis (Steud. ex Sprague) M.G. Gilbert (Loranthaceae) and R. officinalis. Antioxidant activity was observed for C. oblongifolia, M. communis, and P. regularis.

Conclusion: The results justified the use of some investigated plants in the Yemeni ethnomedicine. These findings demonstrated that some of the investigated plants could be a source of new cytotoxic and antibiotic compounds; however, further work is needed.     

Ridaifen-SB8, a novel tamoxifen derivative,induces apoptosis via reactive oxygen species-dependent signaling pathway

Tamoxifen is an anticancer agent widely used for treatment of estrogen receptor (ERα)-positive breast cancer. We previously developed a novel synthesis of tamoxifen and its derivatives, named Ridaifens (RIDs). Some of them, including RID-SB8, exhibited a stronger anticancer activity than tamoxifen in ERα-positive MCF-7 cells while having lost the affinity for ERα, suggesting an ERα-independent anticancer mode of action. In this study, we investigated the underlying mechanism by which RID-SB8 exerts anticancer activity. As expected, anticancer activity of RID-SB8 was not influenced upon knockdown of ERα expression in MCF-7 cells. RID-SB8 exerted similar anticancer effects on thirteen ERα-negative cancer cell lines including human gliosarcoma SF539 cells. In SF539 cells, RID-SB8 triggered loss of mitochondrial membrane potential (ΔΨ_m) and progression of apoptosis accompanied by activation of caspases and translocation of apoptosis-inducing factor (AIF) to the nucleus. Furthermore, it induced reactive oxygen species (ROS), and a ROS scavenger, N-acetylcysteine (NAC), canceled loss of ΔΨ_m and progression of apoptosis triggered by RID-SB8. Using fifteen human cancer cell lines, we demonstrated a significant correlation between RID-SB8 concentration required for ROS production and that required for cytotoxic effect across these cell lines, but such correlation was not observed for tamoxifen. Finally, the selective induction of ROS and cytotoxic effect on cancer cells by RID-SB8 were confirmed. From these results, we concluded that RID-SB8 exerts an anticancer effect via a mode of action distinct from tamoxifen, and that RID-SB8 could become a promising anticancer lead compound which selectively induces ROS formation and apoptosis in cancer cells.     

Potent anti-proliferative effects against oral and cervical cancers of Thai medicinal plants selected from the Thai/Lanna medicinal plant recipe database “MANOSROI III”

Abstract

Context: Thai/Lanna medicinal plant recipes have been used for the treatment of several diseases including oral and cervical cancers.

Objective: To investigate anti-proliferative activity on human cervical (HeLa) and oral (KB) cancer cell lines of medicinal plants selected from Thai/Lanna medicinal plant recipe database “MANOSROI III”.

Materials and methods: Twenty-three methanolic plant crude extracts were tested for phytochemicals and anti-proliferative activity on HeLa and KB cell lines for 24?h by the sulforhodamine B (SRB) assay at the doses of 1?×?10¹–1?×?10^?6?mg/ml. The nine extracts with the concentrations giving 50% growth inhibition (GI₅₀) lower than 100?µg/ml were further semi-purified by liquid/liquid partition in order to evaluate and enhance the anti-proliferative potency.

Results: All extracts contained steroids/triterpenoids, but not xanthones. The methanolic extracts of Gloriosa superba L. (Colchinaceae) root and Albizia chinensis (Osbeck) Merr. (Leguminosae–Mimosoideae) wood gave the highest anti-proliferative activity on HeLa and KB cell lines with the GI₅₀ values of 0.91 (6.0- and 0.31-fold of cisplatin and doxorubicin) and 0.16?µg/ml (28.78- and 82.29-fold of cisplatin and doxorubicin), respectively. Hexane and methanol–water fractions of G. superba exhibited the highest anti-proliferative activity on HeLa and KB cell lines with the GI₅₀ values of 0.15 (37- and 1.9-fold of cisplatin and doxorubicin) and 0.058?µg/ml (77.45- and 221.46-fold of cisplatin and doxorubicin), respectively.

Discussion and conclusion: This study has demonstrated the potential of plants selected from MANOSROI III database especially G. superba and A. chinensis for further development as anti-oral and cervical cancer agents.     

Cytotoxic effects of Eryngium kotschyi and Eryngium maritimum on Hep2, HepG2, Vero and U138 MG cell lines

Abstract

Context: Eryngium maritimum L. and the endemic Eryngium kotschyi Boiss. of the Apiaceae family are used for antiinflammatory, antivenom, antinociceptive and diuretic purposes in folk medicine in Turkey.

Objective: This study investigated the cytotoxic effects of the plant extracts belonging to Eryngium L. genus on various cell lines.

Materials and methods: Cytotoxic activites of the lyophilized aqueous aereal and root parts of the plant extracts on human hepatocellular carcinoma (HepG2), human laryngeal epidermoid carcinoma (Hep2), human glioma (U138-MG) and African green monkey kidney epithelial (Vero) cell lines at 8.33–266.62?µg/ml concentrations were analyzed by lactate dehydrogenase (LDH) leakage and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) (MTT) cell viability assays.

Results: Inhibitory concentration 50 (IC₅₀) values were found <100?µg/ml in most cases varying around 16.33–125.66?µg/ml. IC₅₀ values for E. kostchyi and E. maritimum root parts on Hep2 cells (32.86 and 30.25?µg/ml, respectively), E. kotschyi aereal, E. maritimum aereal and root parts on HepG2 cells (31.75, 32.42 and 35.01?µg/ml, respectively) by MTT assay were found to be close to the US National Cancer Institute (NCI) recommendations (IC₅₀?<?30?µg/ml) to define the antivity aganist cancer cells. The lowest IC₅₀ values according to the LDH method were observed in Hep2 cells and the highest in U138-MG cells. Root parts were found to be more toxic than aereal parts for both plants in both methods in general.

Discussion and conclusion: Both plant extracts exerted cytotoxic activity aganist Hep2 and HepG2 cells, with low IC₅₀ values defining their promising anticancer property according to NCI; however, further analysis are needed to confirm their activity.     

Evaluation of Cytotoxic and Mutagenic Effects of Coriolus versicolor and Funalia trogii Extracts on Mammalian Cells

This study examined the in vitro cytotoxic activities of standardized aqueous bioactive extracts prepared from Coriolus versicolor and Funalia trogiiATCC 200800 on HeLa and fibroblast cell lines using a MTT (3-[4,5-dimetiltiazol-2-]-2–5-difeniltetrazolium bromide) cytotoxicity assay. F. trogii and C. versicolor extracts were cytotoxic to both cell lines. At 10 μL treatment level, F. trogii and C. versicolor extracts inhibited proliferation of HeLa cancer cells by 71.5% and 45%, respectively, compared with controls. Toxicity was lower toward normal fibroblasts. In the latter case, treatment at 10 μL level with F. trogii and C. versicolor extracts reduced cell proliferation by 51.3% and 38.7%, respectively. In separate experiments, the mitotic index (MI) obtained with 3 μL treatment level of unheated extracts of the two fungi was comparable to the MI value obtained by treatment with 4 μg/mL MMC (anticancer agent mitomycin-C). A significant induction of sister chromatid exchange (SCE) was observed in normal cultured lymphocytes treated with MMC (4 μg/mL). MMC treatment reduced replication index compared with treatment with unheated F. trogii extract and negative controls (p < 0.001). In contrast to MMC, F. trogii extracts did not affect the proliferation of human lymphocytes compared with controls (p > 0.05). Laccase and peroxidase enzyme activities in F. trogii extract were implicated in their inhibitory effect on cancer cells. F. trogii extract was concluded to have antitumor activity.     

Cytotoxicity and Structure-activity Relationships of Naphthyridine Derivatives in Human Cervical Cancer,Leukemia, and Prostate Cancer

Naphthyridine compounds are important, because they exhibit various biological activities including anticancer, antimicrobial, and anti-inflammatory activity. Some naphthyridines have antimitotic effects or demonstrate anticancer activity by inhibiting topoisomerase II. These compounds have been investigated as potential anticancer agents, and several compounds are now part of clinical trials. A series of naphthyridine derivatives were evaluated for their in vitro cytotoxic activities against human cervical cancer (HeLa), leukemia (HL-60), and prostate cancer (PC-3) cell lines using an MTT assay. Some compounds (14, 15, and 16) were more potent than colchicine against all three human cancer cell lines and compound (16) demonstrated potency with IC₅₀ values of 0.7, 0.1, and 5.1 µM, respectively. Comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were used for quantitative structure-activity relationship (QSAR) molecular modeling of these compounds. We obtained accurate and predictive three-dimensional QSAR (3D-QSAR) models as indicated by the high PLS parameters of the HeLa (q², 0.857; r², 0.984; r²_pred, 0.966), HL-60 (q², 0.777; r², 0.937; r²_pred, 0.913), and PC-3 (q², 0.702; r², 0.983; r²_pred, 0.974) cell lines. The 3D-QSAR contour maps suggested that the C-1 NH and C-4 carbonyl group of the naphthyridine ring and the C-2 naphthyl ring were important for cytotoxicity in all three human cancer cell lines.     

Chemical composition,antioxidant, antitumor,anticancer and cytotoxic effects of Psidium guajava leaf extracts

Context Psidium guajava L. (Myrtaceae) leaves are used in traditional medicines for the treatment of cancer, inflammation and other ailments.

Objective The current study explores scientific validation for this traditional medication.

Materials and methods We used ferric-reducing antioxidant power (FRAP) and 2,2-diphenyl-1-picryl hydrazil (DPPH) assays to estimate antioxidant activity of P. guajava leaf extracts (methanol, hexane and chloroform). Antitumour and in vivo cytotoxic activities were determined using potato disc assay (PDA) and brine shrimp lethality assay, respectively. Three human carcinoma cell lines (KBM5, SCC4 and U266) were incubated with different doses (10–100?μg/mL) of extracts and the anticancer activity was estimated by MTT assay. NF-κB suppressing activity was determined using electrophoretic mobility shift assay (EMSA). Chemical composition of the three extracts was identified by GC-MS. Total phenolic and flavonoid contents were measured by colorimetric assays.

Results and discussions The order of antioxidant activity of three extracts was methanol?>?chloroform?>?hexane. The IC₅₀ values ranged from 22.73 to 51.65?μg/mL for KBM5; 22.82 to 70.25?μg/mL for SCC4 and 20.97 to 89.55?μg/mL for U266 cells. The hexane extract exhibited potent antitumour (IC_50? value?=_?65.02?μg/mL) and cytotoxic (LC_50? value?=_?32.18?μg/mL) activities. This extract also completely inhibited the TNF-α induced NF-κB activation in KBM5 cells. GC-MS results showed that pyrogallol, palmitic acid and vitamin E were the major components of methanol, chloroform and hexane extracts. We observed significant (p?<?0.05) difference in total phenolic and flavonoid contents of different solvent extracts.

Conclusion The present study demonstrates that P. guajava leaf extracts play a substantial role against cancer and down-modulate inflammatory nuclear factor kB.     

Anastatica hierochuntica (L.) methanolic and aqueous extracts exert antiproliferative effects through the induction of apoptosis in MCF-7 breast cancer cells

Breast cancer therapy using anticancer bioactive compounds derived from natural products as adjuvant treatment has gained recognition due to expensive and toxic conventional chemotherapeutic drugs. The whole plant of Anastatica hierochuntica (L.) (A. hierochuntica) has been investigated for its pharmacologically important anticancer properties but without categorizing the biological activities of the plant parts. We assessed the anticancer potential of different parts of A. hierochuntica (seeds, stems and leaves) and explored their mechanisms of action using the human breast cancer cell line, MCF-7. Currently, we investigated the antiproliferative effects of methanolic (MSD, MST, ML) and aqueous (ASD, AST, AL) extracts of A. hierochuntica plant parts on the MCF-7 cells using cell viability assays. Flow cytometry, Western Blot, DNA fragmentation, and gene expression assays were performed to evaluate apoptosis and cell cycle regulatory proteins. The results indicate that the methanolic and aqueous extracts decreased MCF-7 cell viability in a dose-dependent manner. The induction of apoptosis was observed in all the methanolic and aqueous-treated MCF-7 cells. The cell death process was confirmed by the visualization of DNA fragmentation and cleavage of the intrinsic apoptotic pathways, caspase-9 and caspase-3, the key enzyme causing apoptosis hallmarks. In addition, the most pro-apoptotic extracts, ASD and ML, up-regulated the expression of pro-apoptotic Bax, tumor suppressor TP53 genes and the cyclin inhibitor CDKN1A gene. In conclusion, of the aqueous and methanolic extracts of A. hierochuntica plant parts exerting antiproliferative effects through the induction of apoptosis in breast cancer MCF-7 cells, ASD and ML extracts were the most promising natural-based drugs for the treatment of breast cancer.     

Anti‐inflammatory and anticancer compounds isolated from Ventilago madraspatana Gaertn., Rubia cordifolia Linn. and Lantana camara Linn.

Objectives The aim was to search for anti‐inflammatory and anticancer compounds from three medicinal plants, viz. Ventilago madraspatana Gaertn., Rubia cordifolia Linn. and Lantana camara Linn. Methods The NO? scavenging potential of selected plant extracts was determined on LPS/IFN‐γ activated murine peritoneal macrophage cultures, and iNOS and COX‐2 expression was evaluated by Western blot analysis. Bio‐assay guided fractionation yielded four compounds: physcion and emodin from V. madraspatana, 1‐hydroxytectoquinone from R. cordifolia, and oleanonic acid from L. camara. The anti‐inflammatory activity of these compounds was tested through the carrageenan‐induced rat‐paw oedema model. They were then tested against a murine tumour (Ehrlich ascites carcinoma), and three human cancer cell lines, namely A375 (malignant skin melanoma), Hep2 (epidermoid laryngeal carcinoma) and U937 (lymphoma). Key findings All four compounds dose dependently inhibited NO? through suppression of iNOS protein without affecting macrophage viability. Physcion and emodin caused 65–68% reduction of oedema volume at 40 mg/kg, which validated their in‐vivo anti‐inflammatory effect. 1‐hydroxytectoquinone and oleanonic acid exhibited promising cytotoxicity against A375 cells. Conclusions Ethnomedical reports on these traditional medicinal plants have been rationalised through an insight into the anti‐inflammatory as well as anticancer potential of four constituents, characterised to be prospective candidates for designing novel therapeutic agents.     

Antitumour activity of 3-chlorodeoxylapachol, a naphthoquinone from Avicennia germinans collected from an experimental plot in southern Florida

As part of an ongoing collaborative effort to discover new anticancer agents from plants, an extract obtained from the leaves and twigs of Avicennia germinans, collected in a coastal area of southern Florida, was identified as possessing cytotoxic activity in a panel of human cancer cell lines. Fractionation of the petroleum ether partition, using cytotoxicity to guide the fractionation, led to the isolation of 3-chlorodeoxylapachol. The antitumour potential of 3-chlorodeoxylapachol was demonstrated with the in-vivo hollow fibre assay, a model of antitumour activity using human cancer cell-filled fibres implanted into mice. The possibility that this compound is an artefact of the isolation procedure was ruled out by liquid chromatography-mass spectrometry analysis of extracts prepared without the use of chlorinated solvent. In conclusion, 3-chlordeoxylapachol, a secondary metabolite obtained from the chloroform-soluble extract of a mangrove tree, was cytotoxic in a panel of human cancer cells, and active against KB human cancer cells in the murine hollow fibre antitumour model, with selectivity in KB cells for the intravenous site at lower doses, indicating possible metabolic activation.     

Correlation Between Antioxidative Power and Anticancer Activity in Herbs from Traditional Chinese Medicine Formulae with Anticancer Therapeutic Effect

Abstract

Lobeliae chinensis. Herba (“ban bian lian”), Rheum officinale. Baill. (“da huang”), Sanguisorba officinalis. Linn. (“di yu”), Agrimonia pilosa. Ledeb. (“xian he cao”), and Paris polyphylla. Smith (“zhi hua tou”) are well-known traditional Chinese medicines. They are commonly used in traditional Chinese medicine formulae against cancer. In this study, the antioxidant and anticancer effects of water extracts of these herbs were investigated. In the antioxidant and anticancer studies, water extracts of di yu, xian he cao, and da huang were show to be the most antioxidative and had the highest growth inhibitory effect on human lung adenocarcinoma A549 cell and human breast cancer MCF-7 cell. By comparing their percentage free radical scavenging capacity (SR%) and percentage growth inhibition on A549 and MCF-7 cells, a positive linear relationship between antioxidant activity and anticancer effect of the five herbal water extracts was found. This suggested that the antioxidants of the herbal water extracts might contribute to their anticancer effects on A549 and MCF-7 cells.